2. Signaling Pathways
  3. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  4. EGFR

EGFR

Epidermal growth factor receptor; ErbB-1; HER1

EGFR

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The EGFR family of receptor tyrosine kinases (RTK) comprises four distinct receptors: the EGFR (also known as ErbB-1/HER1), ErbB-2 (neu, HER2), ErbB-3 (HER3) and ErbB-4 (HER4). All EGFR family members are characterized by a modular structure consisting of an extracellular ligand-binding domain, a single hydrophobic transmembrane region, and the intracellular part harbouring the highly conserved tyrosine kinase domain. The ErbB family of receptor tyrosine kinases (RTKs) couples binding of extracellular growth factor ligands to intracellular signaling pathways regulating diverse biologic responses, including proliferation, differentiation, cell motility, and survival. Ten growth factors and their ErbB specificities are: EGF, amphiregulin (AR), and TGF bind ErbB-1; betacellulin, and epiregulin bind both ErbB-1 and ErbB-4; the neuregulins (also called heregulins and Neu differentiation factors) NRG-1 and NRG-2 bind ErbB-3 and ErbB-4; and NRG-3 and NRG-4 bind ErbB-4. No known ligand binds ErbB-2. The three best characterized signaling pathways induced through ErbBs are Ras-mitogen-activated protein kinase (Ras-MAPK), phosphatidylinositol 3 kinase-protein kinase B (PI3K-PKB/Akt), and phospholipase C-protein kinase C (PLC-PKC) pathways.

EGFR Isoform Specific Products:

EGFR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-143246
    EGFR kinase inhibitor 1
    		Inhibitor
    EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
    EGFR kinase inhibitor 1
  • HY-129510
    4-Methyl erlotinib
    		Inhibitor
    4-Methyl erlotinib, is a potent and selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. 4-Methyl erlotinib potently inhibits EGF-mediated tumor cell mitosis by reducing EGFr-specific tyrosine phosphorylation. Using a mouse model of human tumor transplantation, 4-Methyl erlotinib demonstrated significant and sustained suppression of EGFr phosphotyrosine levels, resulting in significant growth inhibition of EGFr-dependent human cancers.
    4-Methyl erlotinib
  • HY-146136
    EGFR-IN-56
    		Inhibitor
    EGFR-IN-56 (Compound 13a) is a potent EGFR inhibitor with IC50 values of 541.7 nM and 132.1 nM against EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-56 blocks cancer cells in G2/M phase and induce into late apoptosis.
    EGFR-IN-56
  • HY-RS04471
    Erbb3 Rat Pre-designed siRNA Set A
    		Inhibitor

    Erbb3 Rat Pre-designed siRNA Set A contains three designed siRNAs for Erbb3 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Erbb3 Rat Pre-designed siRNA Set A
  • HY-147794
    CDK9-IN-41
    		Inhibitor 98.84%
    CDK9-IN-41 is a potent CDK9, EGFR, HER2, and COX-2 kinases inhibitor with IC50s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells.
    CDK9-IN-41
  • HY-161031
    EGFR-IN-93
    		Inhibitor
    EGFR-IN-93 (compound 18) is an allosteric inhibitor of T790M/L858R double mutant EGFR. EGFR-IN-93 can be used for non-small lung cancer (NSCLC) research.
    EGFR-IN-93
  • HY-151154
    EGFR/HER2/DHFR-IN-1
    		Inhibitor
    EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis.
    EGFR/HER2/DHFR-IN-1
  • HY-157526
    EGFR-TK-IN-1
    		Inhibitor
    EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFRL858R/T790M and EGFRDel19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis.
    EGFR-TK-IN-1
  • HY-149846
    SIQ17
    		Inhibitor
    SIQ17 is an EGFR inhibitor that inhibits its activity by occupying the ATP-binding site, with IC50 of 0.62 nM. SIQ17 shows more effective EGFR-TK inhibitory activity compared to the known inhibitor Erlotinib (HY-50896) (IC50 of ∼20 nM). SIQ17 can be used for cancer research
    SIQ17
  • HY-163657
    HER2-IN-20
    		Inhibitor
    HER2-IN-20 (compound 32) is a potent and selective HER2WT and HER2YVMA inhibitor with IC50 values of 49, 42 nM, respectively. HER2-IN-20 has the potential for the research of non-small cell lung cancer (NSCLC).
    HER2-IN-20
  • HY-147798
    EGFR/HER2/CDK9-IN-3
    		Inhibitor
    EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-3
  • HY-172414
    Andamertinib
    		Inhibitor
    Andamertinib is the inhibitor for EGFR and exhibits antineoplastic activity.
    Andamertinib
  • HY-172156
    EGFR-TK-IN-5
    		Inhibitor
    EGFR-TK-IN-5 (Compound NCE 2) is a thiazolyl-pyrazoline derivative. EGFR-TK-IN-5 exhibits strong inhibitory activity and stability against EGFR. EGFR-TK-IN-5 can be used in the study of cancer.
    EGFR-TK-IN-5
  • HY-162148
    HNPMI
    		Inhibitor 99.57%
    HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis.
    HNPMI
  • HY-172897
    EGFR/DHFR-IN-2
    		Inhibitor
    EGFR/DHFR-IN-2 (9b) is a dual h-DHFR/EGFRTK inhibitor, with IC50 values of 0.192 μM and 0.109 μM for h-DHFR and EGFR, respectively. EGFR/DHFR-IN-2 (9b) halts the cell cycle at the G1/S phase and induces apoptosis. EGFR/DHFR-IN-2 (9b) is a potential inhibitor of CYP2C9 and CYP3A4. EGFR/DHFR-IN-2 (9b) can be used in the cancer research.
    EGFR/DHFR-IN-2
  • HY-142519
    EGFR-IN-27
    		Inhibitor
    EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511).
    EGFR-IN-27
  • HY-147796
    EGFR/HER2/CDK9-IN-1
    		Inhibitor
    EGFR/HER2/CDK9-IN-1 (Compound 4) is a potent inhibitor of EGFR/HER2/CDK9 with IC50s of 90.17, 131.39, and 67.04 nM, respectively. EGFR/HER2/CDK9-IN-1 exhibits remarkable antitumor activity.
    EGFR/HER2/CDK9-IN-1
  • HY-162602
    EGFR-IN-115
    		Inhibitor
    EGFR-IN-115 (H-13) is an EGFR inhibitor, with IC50 of 395.2 nM. EGFR-IN-115 can be used in anti-cancer research.
    EGFR-IN-115
  • HY-172179
    EGFR/VEGFR2-IN-5
    		Inhibitor
    EGFR/VEGFR2-IN-5 (Compound 14) is an orally active dual inhibitor of EGFR and VEGFR2 with an IC50 value of 1.15 µM for VEGFR2 and an IC50 value of 0.28 μM for EGFRT790M. EGFR/VEGFR2-IN-5 has significant anticancer activity.
    EGFR/VEGFR2-IN-5
  • HY-163418
    HER2-IN-17
    		Inhibitor
    HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC).
    HER2-IN-17
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
EGFR Isoform Comparison

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